Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:6.2.1.1 (
ACS
)
78,556
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Recently, the
glutathione S-transferase omega 1
(
GSTO1
) is suspected to be involved in certain cancers and neurodegenerative diseases. However, profound investigation on the pathological roles of
GSTO1
has been hampered by the lack of specific methods to determine or modulate its activity in biological systems containing other isoforms with similar catalytic function. Here, we report a fluorescent compound that is able to inhibit and monitor the activity of
GSTO1
. We screened 43 fluorescent chemicals and found a compound (6) that binds specifically to the active site of
GSTO1
. We observed that compound 6 inhibits
GSTO1
by covalent modification but spares other isoforms in HEK293 cells and demonstrated that compound 6 could report the activity of
GSTO1
in NIH/3T3 or HEK293 cells by measuring the fluorescence intensity of the labeled amount of
GSTO1
in SDS-PAGE. Compound 6 is a useful tool to study
GSTO1
, applicable as a specific inhibitor and an activity reporter.
ACS
Chem Biol 2010 May 21
PMID:Isozyme-specific fluorescent inhibitor of glutathione s-transferase omega 1. 2020 72